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Assay Detail

CHEMBL650295

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Adrenal cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-1 angiotensin II receptor (CHEMBL3374)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
Yanagisawa H, Amemiya Y, Kanazaki T, Shimoji Y, Fujimoto K, Kitahara Y, Sada T, Mizuno M, Ikeda M, Miyamoto S, Furukawa Y, Koike H.
J Med Chem (1996) 39 : 323 -338
PubMed 8568823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.95 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447182 1 8.31
CHEMBL116094 1 8.28
CHEMBL115946 1 8.16
CHEMBL1516 OLMESARTAN 3.0 1 8.09
CHEMBL115273 1 8.04
CHEMBL320135 1 8.02
CHEMBL419762 1 7.96
CHEMBL115021 1 7.92
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 7.66
CHEMBL113714 1 7.55
CHEMBL333155 1 7.55
CHEMBL112414 1 7.52
CHEMBL114527 1 7.43
CHEMBL115206 1 7.34
CHEMBL114752 1 7.30
CHEMBL116102 1 7.29
CHEMBL417366 1 7.24
CHEMBL324729 1 7.22
CHEMBL116054 1 7.00
CHEMBL441649 1 7.00
CHEMBL114788 1 6.96
CHEMBL115392 1 6.96
CHEMBL191 LOSARTAN 4.0 1 6.92
CHEMBL49170 1 6.89
CHEMBL326400 1 6.70
CHEMBL115393 1 6.57
CHEMBL300186 1 6.50
CHEMBL323819 1 6.44
CHEMBL274447 1 6.31
CHEMBL113040 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447182 IC50 = 4.9 nM 8.31
CHEMBL116094 IC50 = 5.3 nM 8.28
CHEMBL115946 IC50 = 6.9 nM 8.16
CHEMBL1516 OLMESARTAN IC50 = 8.1 nM 8.09
CHEMBL115273 IC50 = 9.1 nM 8.04
CHEMBL320135 IC50 = 9.5 nM 8.02
CHEMBL419762 IC50 = 11.0 nM 7.96
CHEMBL115021 IC50 = 12.0 nM 7.92
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 22.0 nM 7.66
CHEMBL333155 IC50 = 28.0 nM 7.55
CHEMBL113714 IC50 = 28.0 nM 7.55
CHEMBL112414 IC50 = 30.0 nM 7.52
CHEMBL114527 IC50 = 37.0 nM 7.43
CHEMBL115206 IC50 = 46.0 nM 7.34
CHEMBL114752 IC50 = 50.0 nM 7.30
CHEMBL116102 IC50 = 51.0 nM 7.29
CHEMBL417366 IC50 = 58.0 nM 7.24
CHEMBL324729 IC50 = 60.0 nM 7.22
CHEMBL116054 IC50 = 100.0 nM 7.00
CHEMBL441649 IC50 = 100.0 nM 7.00
CHEMBL114788 IC50 = 110.0 nM 6.96
CHEMBL115392 IC50 = 110.0 nM 6.96
CHEMBL191 LOSARTAN IC50 = 120.0 nM 6.92
CHEMBL49170 IC50 = 130.0 nM 6.89
CHEMBL326400 IC50 = 200.0 nM 6.70
CHEMBL115393 IC50 = 270.0 nM 6.57
CHEMBL300186 IC50 = 320.0 nM 6.50
CHEMBL323819 IC50 = 360.0 nM 6.44
CHEMBL274447 IC50 = 490.0 nM 6.31
CHEMBL113040 IC50 = 600.0 nM 6.22
CHEMBL439743 IC50 = 840.0 nM 6.08
CHEMBL52601 IC50 = 2700.0 nM 5.57
CHEMBL326086 IC50 = 4600.0 nM 5.34
CHEMBL115560 IC50 = 14000.0 nM 4.85
CHEMBL53322 IC50 = 20000.0 nM 4.70
CHEMBL112637 IC50 = 45000.0 nM 4.35